Encapsulation of Morin in Lipid Core/PLGA Shell Nanoparticles Significantly Enhances its Anti-Inflammatory Activity and Oral Bioavailability

Morin (3,5,7,2′,4′-pentahydroxyflavone; MR) is a bioactive plant polyphenol whose therapeutic efficacy is hindered by its poor biopharmaceutical properties. The purpose of this study was to develop a nanoparticle (NP) formulation to enhance the bioactivity and oral bioavailability of MR. The nanoprecipitation technique was employed to encapsulate MR in lipid-cored poly(lactide-co-glycolide) (PLGA) NPs. The optimal NPs were about 200 nm in size with an almost neutral surface charge and a loading efficiency of 82%. The NPs exhibited sustained release of MR within 24 h. In vitro antioxidant assays showed that MR encapsulation did not affect its antioxidant activity.

On the other hand, anti-inflammatory assays in lipopolysaccharide-stimulated macrophages revealed a superior anti-inflammatory activity of MR NPs compared to free MR. Furthermore, oral administration of MR NPs to mice at a single dose of 20 mg/kg MR achieved a 5.6-fold enhancement in bioavailability and a prolongation of plasma half-life from 0.13 to 0.98 h. The results of this study present a promising NP formulation for MR which can enhance its oral bioavailability and bioactivity for the treatment of different diseases such as inflammation.

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Materials

MR was obtained from TCI (Japan). PLGA (lactide/glycolide ratio of 50:50 and MW of 5−10 kDa) was obtained from Acros Organics (Fisher Scientific, USA). Span 80 and 2,2-diphenyl-1-picrylhydrazyl (DPPH) were procured from Sigma-Aldrich (USA). Dimethyl sulfoxide (DMSO), potassium bromide (KBr), acetone (absolute) and ethanol (absolute) were purchased from Fisher Chemical (UK). Capryol 90 (CP90) was a kind gift from Gattefossé (France). Olive oil (extra virgin) was purchased from a local supermarket (Jordan). Castor oil (BP) was obtained from Philadelphia Pharmaceuticals (Jordan). Tween 80 was obtained from RFCL Ltd (India). Phosphate buffered saline (PBS, 10×) was purchased from Fisher Bioreagents (Belgium). Lipopolysaccharide (LPS; E. coli O55:B5) was obtained from Santa Cruz Biotechnology Inc. (USA). Type 1 ultrapure water was used throughout the experiments.

Suhair Sunoqrot, Malak Alkurdi, Abdel Qader Al Bawab, Alaa M. Hammad, Rabab Tayyem, Ali Abu Obeed, Mohammed Abufara, Encapsulation of Morin in Lipid Core/PLGA Shell Nanoparticles Significantly Enhances its Anti-Inflammatory Activity and Oral Bioavailability, Saudi Pharmaceutical Journal, 2023, ISSN 1319-0164, https://doi.org/10.1016/j.jsps.2023.04.010.

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